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Solubility of cilostazol in the presence of polyethylene glycol 4000, polyethylene glycol 6000, polyvinylpyrrolidone K30, and poly(1-vinylpyrrolidone-co-vinyl acetate) at different temperatures

Authors :
Dong-Hyeon Ha
Min-Soo Kim
Hee Jun Park
Jeong-Soo Kim
Do-Hoon Kuk
Woo-Yong Sim
In-hwan Baek
Eun-Sol Ha
Source :
The Journal of Chemical Thermodynamics. 113:6-10
Publication Year :
2017
Publisher :
Elsevier BV, 2017.

Abstract

The solubilities of cilostazol in aqueous solutions containing polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), polyvinylpyrrolidone K30 (PVP K30), and poly(1-vinylpyrrolidone-co-vinyl acetate) (PVP/VA) are measured at temperatures ranging from 298.15 to 318.15 K. It increased with the increase in the hydrophilic carrier concentration and temperature. PVP/VA was the most effective polymer to solubilize cilostazol. The transfer Gibbs free energy (Δ tr G °) and enthalpy (Δ tr H °) values were negative, indicating that the transfer of cilostazol from only water to an aqueous hydrophilic polymer solution is spontaneous and energetically favorable. Furthermore, the Δ tr G ° and Δ tr H ° values decreased with the increase in the hydrophilic polymer concentration, indicating that solubilization is more favorable with the increase in the hydrophilic polymer concentrations. In particular, the Δ tr G ° values considerably decreased for PVP/VA compared to PEG 4000, PEG 6000, and PVP K30. This result indicated that PVP/VA is an effective solubilizing additive for developing oral solid formulations of cilostazol.

Details

ISSN :
00219614
Volume :
113
Database :
OpenAIRE
Journal :
The Journal of Chemical Thermodynamics
Accession number :
edsair.doi...........461ce0c51939495f52b8eea62ed5c066
Full Text :
https://doi.org/10.1016/j.jct.2017.05.040